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Dual Inhibition of BACE1 and Aβ Aggregation by β-ecdysone: Application of a Phytoecdysteroid Scaffold in Alzheimer's Disease Therapeutics

Dual Inhibition of BACE1 and Aβ Aggregation by β-ecdysone: Application of a Phytoecdysteroid Scaffold in Alzheimer's Disease Therapeutics

Sandipan Chakraborty, Soumalee Basu

Int J Biol Macromol. 2017 Feb;95:281-287.

PMID: 27871792

Abstract:

Current medications for the complex neurological disorder, Alzheimer's disease (AD), can neither stop disease progression nor revert back disease pathogenesis. The present study demonstrates the applicability of a phytoecdysteroid, β-ecdysone, as a multi-potent agent in AD therapeutics. β-ecdysone strongly binds to the active site cavity of BACE1 with calculated dissociation constant of 1.75±0.1μM. Steady-state and time-resolved fluorescence spectroscopy reveal that binding of β-ecdysone induces conformational transition of the protein from open to closed form thereby blocking substrate binding. Even 500nM of the compound completely blocks the enzyme activity. Furthermore, β-ecdysone strongly inhibits Aβ aggregation, evident from ANS and ThT binding assay. Co-incubation of equimolar peptide and β-ecdysone completely inhibits Aβ fibril formation which is further complemented by the AFM study. Low systemic toxicity of β-ecdysone further extends the applicability of the compound as functional food and dietary supplement for disease management.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP5289747	β-Ecdysone		5289-74-7	Price

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